caa a22 4500 378907085 CHVBK 20180305123532.0 cr unu---uuuuu 161128e20040401xx s 000 0 eng 10.1524/ract.92.4.277.35610 doi (NATIONALLICENCE)gruyter-10.1524/ract.92.4.277.35610 188Re(V)-DMSA: in-vitro and in-vivo studies on the individual stereo isomers [Elektronische Daten] [Stefan Guhlke, S. Scheithauer, K. Oetjen, J. Sartor, H. Bender, H. J. Biersack] The pentavalent rhenium-188 meso-dimercaptosuccinic acid complex 188Re(V)-DMSA is a beta-emitting analogue of Tc99m(V)-DMSA, an established tracer that is taken up in a variety of histological different tumors and especially in bone metastases arising from breast and prostate carcinomas. The similar general biodistribution and tumor avidity of 188Re- and 99mTc(V)-DMSA therefore suggests the use of the rhenium analog as an agent for therapeutic applications. No-carrier-added 188Re(V)-DMSA is composed of a mixture of three stereoisomers arising from different orientations of the 4 carboxylate groups of the complex. For therapeutic applications it must be known whether there is a difference in the in-vivo biodistribution and kinetics of the individual stereo isomers. The aim of this study was therefore a) to characterize the chemical stability of each of the 3 stereoisomers with respect to time, temperature and pH and b) to evaluate if there are differences in the in-vivo organ distribution of the pure isomers compared to the isomeric mixture. The in-vitro results revealed for all three individual isomers of 188Re(V)-DMSA a rather slow (with respect to half-life of Re-188) temperature and pH dependent rate of interconversion which would justify the application of pure isomers. The data obtained from urine samples of rats showed a faster interconversion rate and reached a stable isomer distribution after about six to ten hours, depending on which isomer was injected. However there was no evidence for isomer specific excretion rates. The organ biodistribution patterns of all three isomers were very similar at all times studied (10min up to 24hours p.i). The tumor uptake in a rat mammary carcinoma model at 1hour p.i. did also not show any significant differences. In conclusion the preparation and administration of pure stereoisomers of 188Re-DMSA is possible, however, in-vivo no significant differences in organ distribution and kinetics were observed which would favour the use of purified stereo isomers over the isomeric mixture of 188Re(V)-DMSA. © 2004 Oldenbourg Wissenschaftsverlag GmbH Laboratory techniques, experiments nationallicence Analytical chemistry nationallicence Inorganic chemistry nationallicence Guhlke Stefan aut Scheithauer S. aut Oetjen K. aut Sartor J. aut Bender H. aut Biersack H. J. aut Radiochimica Acta/International journal for chemical aspects of nuclear science and technology Oldenbourg Wissenschaftsverlag GmbH 92/4-6/2004(2004-04-01), 277-283 0033-8230 92:4-6/2004<277 2004 92 ract https://doi.org/10.1524/ract.92.4.277.35610 text/html Onlinezugriff via DOI 1 research article jats NATIONALLICENCE 856 40 https://doi.org/10.1524/ract.92.4.277.35610 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Guhlke Stefan aut NATIONALLICENCE 700 1- Scheithauer S. aut NATIONALLICENCE 700 1- Oetjen K. aut NATIONALLICENCE 700 1- Sartor J. aut NATIONALLICENCE 700 1- Bender H. aut NATIONALLICENCE 700 1- Biersack H. J. aut NATIONALLICENCE 773 0- Radiochimica Acta/International journal for chemical aspects of nuclear science and technology Oldenbourg Wissenschaftsverlag GmbH 92/4-6/2004(2004-04-01), 277-283 0033-8230 92:4-6/2004<277 2004 92 ract CC0 http://creativecommons.org/publicdomain/zero/1.0 nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-gruyter